Abstract
Based on the structures of several lipophilic trioxolane antimalarial prototypes, we set out to determine which functional groups were associated with good antimalarial profiles and identify more polar (lower Log P/Log D) lead compounds with good physicochemical properties. More lipophilic trioxolanes tended to have better oral activities than their more polar counterparts. Trioxolanes with a wide range of neutral and basic, but not acidic, functional groups had good antimalarial profiles.
Original language | English (US) |
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Pages (from-to) | 6368-6382 |
Number of pages | 15 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 14 |
Issue number | 18 |
DOIs | |
State | Published - Sep 15 2006 |
Keywords
- 1,2,4-Trioxolane
- Antimalarial
- Artemisinin
- Secondary ozonide
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry